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PF-04418948

Cat. No. M9232
PF-04418948 Structure
Size Price Availability Quantity
5mg USD 67.5  USD75 In stock
10mg USD 96.3  USD107 In stock
25mg USD 234  USD260 In stock
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Quality Control
Biological Activity

PF-04418948 inhibited prostaglandin E(2)(PGE(2))-induced increase in cAMP in cells expressing EP(2) receptors with a functional K(B) value of 1.8 nM. In human myometrium, PF-04418948 produced a parallel, rightward shift of the butaprost-induced inhibition of the contractions induced by electrical field stimulation with an apparent K(B) of 5.4 nM. In dog bronchiole and mouse trachea, PF-04418948 produced parallel rightward shifts of the PGE(2)-induced relaxation curve with a K(B) of 2.5 nM and an apparent K(B) of 1.3 nM respectively. Reversal of the PGE(2)-induced relaxation in the mouse trachea by PF-04418948 produced an IC(50) value of 2.7 nM.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 409.41
Formula C23H20FNO5
CAS Number 1078166-57-0
Purity 99.67%
Solubility DMSO: ≥ 50 mg/mL
Storage at -20°C
References

Selectivity profiling of the novel EP2 receptor antagonist, PF-04418948, in functional bioassay systems: atypical affinity at the guinea pig EP2 receptor.
Birrell MA, et al. Br J Pharmacol. 2013 Jan;168(1):129-38. PMID: 22747912.

In vitro and in vivo characterization of PF-04418948, a novel, potent and selective prostaglandin EP₂ receptor antagonist.
af Forselles KJ, et al. Br J Pharmacol. 2011 Dec;164(7):1847-56. PMID: 21595651.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: PF-04418948 supplier, Prostaglandin Receptor, inhibitors

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